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PKI 14-22 amide,myristoylated
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PKI 14-22 amide,myristoylated图片
CAS NO:201422-03-9
包装:1mg
市场价:1350元

产品介绍
PKI 14-22 amide, myristoylated 是一种有效的 cAMP 依赖性 PKA 抑制剂。 PKI 14-22 amide, myristoylated 减少 IgG 介导的吞噬反应，也抑制中性粒细胞粘附。
Cas No.201422-03-9
化学名(S,Z)-N'1-((S,Z)-1-hydroxy-1-(((2S,3S)-1-hydroxy-1-imino-3-methylpentan-2-yl)imino)propan-2-yl)-2-((Z)-((2S,3Z,5S,6Z,9Z,11S,12Z,14S,15Z,18Z)-2,5,14-tris(3-guanidinopropyl)-1,4,7,10,13,16,19-heptahydroxy-11-((R)-1-hydroxyethyl)-3,6,9,12,15,18-hexaazadotria
Canonical SMILESCCCCCCCCCCCCC/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])[C@@](CC)([H])C)([H])C)([H])CC(O)=N)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])[C@@](O)([H])C)([H])CCCNC(N)=N
分子式C53H100N20O12
分子量1209.5
溶解度Soluble to 1 mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Myristoylated PKI (14-22) amide is an effective inhibitor of cAMP-dependent protein kinase (PKA) and blocks hyperalgesia produced by spinal administration of 8-bromo-cAMP. [1]

PKAs are the major mediators of cAMP signaling in eukaryotes. PKAs play an important role in several biological processes such as gene expression, apoptosis, tissue differentiation and cellular proliferation. PKAS play these functions through the phosphorylation of protein substrates at serine/threonine residues. [2]

PKAs play a key role in neutrophil phagocytosis. CAMP/PKAs regulate F-actin reorganization during receptor-mediated phagocytosis, particularly triggered by IgG-FcR interaction. Myristoylated PKI 14-22 amide reduced the IgG-mediated phagocytic response in a manner of dose-dependent. When the concentration is higher than 10 μM, PKI 14-22 amide can inhibit neutrophil adhesion, which make the phagocytosis measurements impossible to perform. [1]

Because the unregulated activity of PKA in mammalian cells has been implicated in the pathogenesis of several types of cancer, the development of PKI (14–22) amide has been pursued as a potential treatment for these types of cancer and many other diseases related with PKAs.[1,2]

References:
[1] Ydrenius L1, Majeed M, etal. , Activation of cAMP-dependent protein kinase is necessary for actin rearrangements in human neutrophils during phagocytosis. J Leukoc Biol. 2000 Apr;67(4):520-8.
[2] Swierczewski BE, Davies SJ.   Developmental regulation of protein kinase A expression and activity in Schistosoma mansoni. Int J Parasitol. 2010 Jul;40(8):929-35.